Millipore Sigma Vibrant Logo

438193 LRRK2-IN-1 - CAS 1234480-84-2 - Calbiochem

LRRK2-IN-1, CAS 1234480-84-2, is a cell-permeable, ATP competitive, selective LRRK2 inhibitor (IC50 = 13, 6 & 2.45 µM for WT, G2019S mutant & drug resistant A2016T mutant LRRK2, respectively).

LRRK2-IN-1 - CAS 1234480-84-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

同义词: LRRK2 Inhibitor I

View Products on Sigmaaldrich.com
438193
查看价格及供货情况

概述

Replacement Information

重要规格表

CAS #Empirical Formula
1234480-84-2C₃₁H₃₈N₈O₃

价格及供货情况

产品目录编号 库存情况包装 数量 / 包装 价格 数量
438193-5MGCN
正在查询供货情况......
—
目前缺货 目前缺货
有货 
停产
少量现货
供货情况有待确认
    其余：另行通知
      其余：另行通知
      另行通知
      联系客户服务
      Contact Customer Service

      		 玻璃瓶 5 mg
      正在检索价格......
      无法检索价格。
      最小订购数量为倍数
      Maximum Quantity is
      以订单确认为准 更多信息
      您节约了 ()。
       
      —
      Request Pricing
      		 —
      Description
      OverviewA cell-permeable, ATP competitive, potent, and selective LRRK2 inhibitor (IC50 of 13 nM, 6 nM, and 2.45 µM for wild type, G2019S mutant, and drug resistant A2016T mutant LRRK2, respectively, in an in vitro ATP-site competititon binding assay). While it is shown to inhibit DCLK2 (IC50 = 45 nM) and suppress MAPK7 autophosphorylation (EC50 = 160 nM), this compound (< 10 µM) demonstrates very good overall selectivity, targeting 12 out of 442 other kinases in a kinase-binding and biochemical assay. At 0.05–3 µM, it induces dose-dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild-type LRRK2 and LRRK2[G2019S] in stably transfected HEK293 cells, but not in the drug-resistant LRRK2[A2016T] and LRRK2[A2016T + G2019S] mutants. Similar effects on endogenous LRRK2 phosphorylation and 14-3-3 binding can be observed in human lympho¬blastoid cells and for the LRRK2 G2019S mutant derived from a Parkinson's disease patient, and in human-derived neuroblastoma SHSY5Y cells, as well as in mouse Swiss 3T3 cells. 100 mg/kg of compound injected into mice elicits complete Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, but not in the brain which may result from an inability to penetrate the blood-brain barrier. In addition, it promotes relocalization of LRRK2 to more aggregate and fibrillar-like structures.
      Catalogue Number438193
      Brand Family Calbiochem®
      SynonymsLRRK2 Inhibitor I
      References
      ReferencesDeng, X., et al. 2011. Nat. Chem. Biol. 7, 203.
      Product Information
      CAS number1234480-84-2
      FormYellow-white to pale yellow powder
      Hill FormulaC₃₁H₃₈N₈O₃
      Chemical formulaC₃₁H₃₈N₈O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationLRRK2-IN-1, CAS 1234480-84-2, is a cell-permeable, ATP competitive, selective LRRK2 inhibitor (IC50 = 13, 6 & 2.45 µM for WT, G2019S mutant & drug resistant A2016T mutant LRRK2, respectively).
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Regulatory Review
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freexe (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      产品目录编号 GTIN
      438193-5MGCN 07790788060954

      Documentation

      LRRK2-IN-1 - CAS 1234480-84-2 - Calbiochem MSDS

      职位

      物料安全数据表 (MSDS) 

      LRRK2-IN-1 - CAS 1234480-84-2 - Calbiochem 分析证书

      标题批号
      438193

      参考

      参考信息概述
      Deng, X., et al. 2011. Nat. Chem. Biol. 7, 203.
      数据表

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision06-September-2011 RFH
      SynonymsLRRK2 Inhibitor I
      DescriptionA cell-permeable, ATP competitive, potent, and selective LRRK2 inhibitor (IC50 of 13 nM, 6 nM, and 2.45 µM for wild type, G2019S mutant, and drug resistant A2016T mutant LRRK2, respectively, in an in vitro ATP-site competititon binding assay). While it is shown to inhibit DCLK2 (IC50 = 45 nM) and suppress MAPK7 autophosphorylation (EC50 = 160 nM), this compound (< 10 µM) demonstrates very good overall selectivity, targeting 12 out of 442 other kinases in a kinase-binding and biochemical assay. At 0.05-3 µM, it induces dose-dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild-type LRRK2 and LRRK2[G2019S] in stably transfected HEK293 cells, but not in the drug-resistant LRRK2[A2016T] and LRRK2[A2016T + G2019S] mutants. Similar effects on endogenous LRRK2 phosphorylation and 14-3-3 binding can be observed in human lympho-blastoid cells and for the LRRK2 G2019S mutant derived from a Parkinson's disease patient, and in human-derived neuroblastoma SHSY5Y cells, as well as in mouse Swiss 3T3 cells. 100 mg/kg of compound injected into mice elicits complete Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, but not in the brain which may result from an inability to penetrate the blood-brain barrier. In addition, it promotes relocalization of LRRK2 to more aggregate and fibrillar-like structures.
      FormYellow-white to pale yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1234480-84-2
      Chemical formulaC₃₁H₃₈N₈O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freexe (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Regulatory Review
      ReferencesDeng, X., et al. 2011. Nat. Chem. Biol. 7, 203.